Lanraplenib monosuccinate (Synonyms: GS-9876 monosuccinate)

Cat. No.: HY-109091A: FAQs
Data Sheet Handling Instructions

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Lanraplenib monosuccinate (GS-9876 monosuccinate) is a highly selective and orally active SYK inhibitor (IC₅₀=9.5 nM) in development for the treatment of inflammatory diseases. Lanraplenib monosuccinate (GS-9876 monosuccinate) inhibits SYK activity in platelets via the glycoprotein VI (GPVI) receptor without prolonging bleeding time (BT) in monkeys or humans.

For research use only. We do not sell to patients.

Lanraplenib monosuccinate Chemical Structure

CAS No. : 1800046-97-2

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Other In-stock Forms of Lanraplenib monosuccinate:

Other Forms of Lanraplenib monosuccinate:

Lanraplenib In-stock
Lanraplenib succinate In-stock

2 Publications Citing Use of MCE Lanraplenib monosuccinate

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

IC50: 9.5 nM (SYK)^[1]

In Vitro

Lanraplenib monosuccinate (GS-9876 monosuccinate) inhibits anti-IgM stimulated phosphorylation of AKT, BLNK, BTK, ERK, MEK, and PKCδ in human B cells with EC₅₀ values of 24-51 nM. Lanraplenib monosuccinate inhibits anti-IgM mediated CD69 and CD86 expression on B-cells (EC₅₀=112±10 nM and 164±15 nM, respectively) and anti-IgM /anti-CD40 co-stimulated B cell proliferation (EC₅₀=108±55 nM). In human macrophages, Lanraplenib monosuccinate inhibits IC-stimulated TNFα and IL-1β release (EC₅₀=121±77 nM and 9±17 nM, respectively)^[1].
Lanraplenib monosuccinate (GS-9876 monosuccinate) inhibits glycoprotein VI (GPVI)-induced phosphorylation of linker for activation of T cells and phospholipase Cγ2, platelet activation and aggregation in human whole blood, and platelet binding to collagen under arterial flow^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

561.59

Formula

C₂₇H₃₁N₉O₅

CAS No.

1800046-97-2

SMILES

NC1=CN=CC(C2=CN3C(C(NC4=CC=C(N5CCN(C6COC6)CC5)C=C4)=N2)=NC=C3)=N1.O=C(O)CCC(O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility

In Vitro:

DMSO : 125 mg/mL (222.58 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.7807 mL	8.9033 mL	17.8066 mL
5 mM	0.3561 mL	1.7807 mL	3.5613 mL
10 mM	0.1781 mL	0.8903 mL	1.7807 mL

View the Complete Stock Solution Preparation Table

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Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (3.70 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (3.70 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Di Paolo J, et al. FRI0049 Preclinical Characterization of GS-9876, A Novel, Oral SYK Inhibitor That Shows Efficacy in Multiple Established Rat Models of Collagen-Induced Arthritis.Annals of the Rheumatic Diseases 2016;75:443-444.

[2]. Clarke AS, et al. Effects of GS-9876, a novel spleen tyrosine kinase inhibitor, on platelet function and systemic hemostasis. Thromb Res. 2018 Oct;170:109-118. [Content Brief]

[3]. Kivitz AJ, et al. GS-9876, a Novel, Highly Selective, SYK Inhibitor in Patients with Active Rheumatoid Arthritis: Safety, Tolerability and Efficacy Results of a Phase 2 Study [abstract]. Arthritis Rheumatol.2018; 70 (suppl 10).

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.7807 mL	8.9033 mL	17.8066 mL	44.5165 mL
	5 mM	0.3561 mL	1.7807 mL	3.5613 mL	8.9033 mL
	10 mM	0.1781 mL	0.8903 mL	1.7807 mL	4.4516 mL
	15 mM	0.1187 mL	0.5936 mL	1.1871 mL	2.9678 mL
	20 mM	0.0890 mL	0.4452 mL	0.8903 mL	2.2258 mL
	25 mM	0.0712 mL	0.3561 mL	0.7123 mL	1.7807 mL
	30 mM	0.0594 mL	0.2968 mL	0.5936 mL	1.4839 mL
	40 mM	0.0445 mL	0.2226 mL	0.4452 mL	1.1129 mL
	50 mM	0.0356 mL	0.1781 mL	0.3561 mL	0.8903 mL
	60 mM	0.0297 mL	0.1484 mL	0.2968 mL	0.7419 mL
	80 mM	0.0223 mL	0.1113 mL	0.2226 mL	0.5565 mL
	100 mM	0.0178 mL	0.0890 mL	0.1781 mL	0.4452 mL

Lanraplenib monosuccinate Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Lanraplenib monosuccinate1800046-97-2GS-9876 monosuccinateSykSpleen tyrosine kinaseInhibitorinhibitorinhibit

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